CA2925497C - Conformationally restricted pi3k and mtor inhibitors - Google Patents

Conformationally restricted pi3k and mtor inhibitors Download PDF

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Publication number
CA2925497C
CA2925497C CA2925497A CA2925497A CA2925497C CA 2925497 C CA2925497 C CA 2925497C CA 2925497 A CA2925497 A CA 2925497A CA 2925497 A CA2925497 A CA 2925497A CA 2925497 C CA2925497 C CA 2925497C
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CA
Canada
Prior art keywords
tetrahydro
pyrimido
pyrrolo
morpholino
oxazin
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CA2925497A
Other languages
English (en)
French (fr)
Other versions
CA2925497A1 (en
Inventor
Vladimir Cmiljanovic
Paul Hebeisen
Eileen JACKSON
Florent Beaufils
Thomas Bohnacker
Matthias Wymann
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Torqur Ag
Universitaet Basel
Original Assignee
Torqur Ag
Universitaet Basel
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Filing date
Publication date
Application filed by Torqur Ag, Universitaet Basel filed Critical Torqur Ag
Publication of CA2925497A1 publication Critical patent/CA2925497A1/en
Application granted granted Critical
Publication of CA2925497C publication Critical patent/CA2925497C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CA2925497A 2013-10-04 2014-10-03 Conformationally restricted pi3k and mtor inhibitors Active CA2925497C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13187386 2013-10-04
EP13187386.1 2013-10-04
PCT/EP2014/071227 WO2015049369A1 (en) 2013-10-04 2014-10-03 Conformationally restricted pi3k and mtor inhibitors

Publications (2)

Publication Number Publication Date
CA2925497A1 CA2925497A1 (en) 2015-04-09
CA2925497C true CA2925497C (en) 2022-12-06

Family

ID=49303818

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2925497A Active CA2925497C (en) 2013-10-04 2014-10-03 Conformationally restricted pi3k and mtor inhibitors

Country Status (17)

Country Link
US (1) US9556203B2 (zh)
EP (1) EP3052504B1 (zh)
JP (1) JP6426745B2 (zh)
KR (1) KR102369925B1 (zh)
CN (1) CN105593231B (zh)
AU (1) AU2014331049B2 (zh)
BR (1) BR112016007122A2 (zh)
CA (1) CA2925497C (zh)
ES (1) ES2721302T3 (zh)
HK (1) HK1220971A1 (zh)
IL (1) IL244708B (zh)
MX (1) MX364558B (zh)
PH (1) PH12016500569B1 (zh)
RU (1) RU2669696C2 (zh)
SG (1) SG11201602602RA (zh)
WO (1) WO2015049369A1 (zh)
ZA (1) ZA201602084B (zh)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3978500B1 (en) 2015-12-16 2023-11-22 Genentech, Inc. Process for the preparation of tricyclic pi3k inhibitor compounds
US10722484B2 (en) 2016-03-09 2020-07-28 K-Gen, Inc. Methods of cancer treatment
PT3458067T (pt) 2016-05-18 2021-04-07 Univ Basel Tratamento de distúrbios neurológicos
JP7108631B2 (ja) 2017-01-06 2022-07-28 パルヴェラ セラピューティクス、インク． ｍＴＯＲ阻害剤の無水組成物およびその使用方法
JP2021530463A (ja) 2018-07-02 2021-11-11 パルヴェラ セラピューティクス、インク． ｍＴＯＲ阻害剤の無水組成物および使用方法

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5543523A (en) 1994-11-15 1996-08-06 Regents Of The University Of Minnesota Method and intermediates for the synthesis of korupensamines
AUPO903897A0 (en) 1997-09-08 1997-10-02 Commonwealth Scientific And Industrial Research Organisation Organic boronic acid derivatives
RU2246496C1 (ru) * 2003-09-12 2005-02-20 Тец Виктор Вениаминович Вещество с противовирусной и антибактериальной активностью на основе производных 2,8-дитиоксо-1h-пирано[2,3-d, 6,5-d`] дипиримидина и их 10-аза-аналогов
US20060188498A1 (en) * 2005-02-18 2006-08-24 Genentech, Inc. Methods of using death receptor agonists and EGFR inhibitors
WO2006125179A1 (en) * 2005-05-19 2006-11-23 Xenon Pharmaceuticals Inc. Tricyclic compounds and their uses as therapeutic agents
ZA200902382B (en) * 2006-10-19 2010-08-25 Signal Pharm Llc Heteroaryl compounds, compositions thereof, and their use as protein kinase inhibitors
FR2933983B1 (fr) * 2008-07-15 2010-08-27 Servier Lab Nouveaux derives tricycliques,leur procede de preparation et les compositions pharmaceutiques qui les contiennent.
TWI378933B (en) * 2008-10-14 2012-12-11 Daiichi Sankyo Co Ltd Morpholinopurine derivatives
US9475812B2 (en) * 2011-06-04 2016-10-25 Xuanzhu Pharma Co., Ltd. Pyridonaphthyridine type dual PI3K and mTOR inhibitor and its preparation and use
CN103030653A (zh) * 2011-09-30 2013-04-10 上海恒瑞医药有限公司 杂芳基并嘧啶类衍生物及其可药用盐、其制备方法及其在医药上的应用

Also Published As

Publication number Publication date
AU2014331049B2 (en) 2018-03-29
EP3052504A1 (en) 2016-08-10
CA2925497A1 (en) 2015-04-09
HK1220971A1 (zh) 2017-05-19
IL244708B (en) 2019-06-30
US9556203B2 (en) 2017-01-31
KR20160067946A (ko) 2016-06-14
US20160244463A1 (en) 2016-08-25
RU2669696C2 (ru) 2018-10-15
PH12016500569A1 (en) 2016-06-13
MX2016004203A (es) 2016-12-16
ZA201602084B (en) 2017-05-31
CN105593231A (zh) 2016-05-18
SG11201602602RA (en) 2016-04-28
JP6426745B2 (ja) 2018-11-21
EP3052504B1 (en) 2019-02-06
ES2721302T3 (es) 2019-07-30
WO2015049369A1 (en) 2015-04-09
BR112016007122A2 (pt) 2017-08-01
NZ718614A (en) 2021-11-26
PH12016500569B1 (en) 2016-06-13
KR102369925B1 (ko) 2022-03-03
CN105593231B (zh) 2018-06-05
JP2016531947A (ja) 2016-10-13
IL244708A0 (en) 2016-04-21
RU2016112164A3 (zh) 2018-05-22
RU2016112164A (ru) 2017-11-09
MX364558B (es) 2019-04-29
AU2014331049A1 (en) 2016-04-28

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